产品
编 号：F409120
分子式：C24H34F3N3O3
分子量：469.54
分子式：C24H34F3N3O3
分子量：469.54
产品类型
规格
价格
是否有货
5mg
2700
In-stock
10mg
5040
In-stock
结构图
CAS No: 624733-88-6
产品详情
生物活性：
MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2.
体内研究：
MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood. Administration of MK0812 at 30 mg/kg, p.o. reduces the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+ neutrophil frequency is observed. In addition, MK0812 treatment causes a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2.
体外研究：
MK-0812 completely blocks all MCP-1 mediated response in a concentration dependent manner, with an IC50 of 3.2 nM. This value is similar to the potency observed for the inhibition of 125I-MCP-1 binding by MK-0812 on isolated monocytes (IC50 4.5 nM). In fact, the antagonist not only completely blocks the shape change response to exogenous MCP-1, but also results in a monocyte forward scatter measurement below unstimulated or basal levels. The addition of MK-0812 to rhesus blood also inhibits MCP-1 induced monocyte shape change. The IC50 for MK-0812 in whole blood assays is 8 nM MK0812 is a potent and selective small molecule CCR2 antagonist.
MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2.
体内研究：
MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood. Administration of MK0812 at 30 mg/kg, p.o. reduces the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+ neutrophil frequency is observed. In addition, MK0812 treatment causes a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2.
体外研究：
MK-0812 completely blocks all MCP-1 mediated response in a concentration dependent manner, with an IC50 of 3.2 nM. This value is similar to the potency observed for the inhibition of 125I-MCP-1 binding by MK-0812 on isolated monocytes (IC50 4.5 nM). In fact, the antagonist not only completely blocks the shape change response to exogenous MCP-1, but also results in a monocyte forward scatter measurement below unstimulated or basal levels. The addition of MK-0812 to rhesus blood also inhibits MCP-1 induced monocyte shape change. The IC50 for MK-0812 in whole blood assays is 8 nM MK0812 is a potent and selective small molecule CCR2 antagonist.
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